| Bioactivity | TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis[1][2]. | ||||||||||||
| Invitro | TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 µM to 1.31 µM[1].TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours[3]. | ||||||||||||
| Name | TAK-243 | ||||||||||||
| CAS | 1450833-55-2 | ||||||||||||
| Formula | C19H20F3N5O5S2 | ||||||||||||
| Molar Mass | 519.52 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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TAK-243
CAS: 1450833-55-2 F: C19H20F3N5O5S2 W: 519.52
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which bl
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